Patents by Inventor Leo Alig

Leo Alig has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4652679
    Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.
    Type: Grant
    Filed: May 9, 1983
    Date of Patent: March 24, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4585796
    Abstract: The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.
    Type: Grant
    Filed: August 1, 1983
    Date of Patent: April 29, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4361578
    Abstract: The invention is directed to 3-oxo-D-homosteroids and derivatives thereof which are useful as antiantigens.
    Type: Grant
    Filed: November 16, 1981
    Date of Patent: November 30, 1982
    Inventors: Leo Alig, Andor Furst, Peter Keller, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4348327
    Abstract: 17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,A is ##STR2## and R.sub.1 is H or CH.sub.3are prepared by hydrating the corresponding 17-nitriles with a mixture of a lower carboxylic acid and its anhydride in the presence of perchloric acid. The resultant 17.beta.-N-acylcarboxamide is then treated with an alkali metal hydroxide in a polyhydric alcohol at an elevated temperature. The product acids are intermediates, e.g., for the production of steroids having antiinflammatory activity.
    Type: Grant
    Filed: June 23, 1981
    Date of Patent: September 7, 1982
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Ulrich Kerb, Rudolf Wiechert, Leo Alig, Andor Furst, Marcel Muller
  • Patent number: 4272630
    Abstract: The present invention is directed to 3-oxo, 6,9-hydro or halo, 11-oxo or (.alpha.--H,.beta.--OH), 17a-alkanoyloxy, 17a.beta.-carboxylate D-homosteroids which are useful as antiinflammatory agents.
    Type: Grant
    Filed: January 11, 1980
    Date of Patent: June 9, 1981
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4252729
    Abstract: The present disclosure is concerned with 9.alpha.-chloro-17-(m-iodobenzyloxy) steroids and a process for their manufacture. The subject compounds are useful as intermediates in the synthesis of pharmacologically-active substances and have themselves been found to exhibit pharmacological activity.
    Type: Grant
    Filed: May 7, 1979
    Date of Patent: February 24, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4202841
    Abstract: D-Homopregnanes of the formula ##STR1## wherein the dotted line in the 1,2-position together with the corresponding solid line denotes a single or double carbon-carbon bond; R.sup.6 is hydrogen, fluoro, chloro or methyl; R.sup.9 is hydrogen, fluoro, chloro or bromo; R.sup.11 is hydroxyl, acyloxy, fluoro or chloro; and R.sup.17a is hydroxyl or acyloxy with the proviso that when R.sup.9 is fluoro, chloro or bromo and R.sup.11 is fluoro or chloro, the atomic number of R.sup.11 is less than or equal to that of R.sup.9 ; and with the further proviso that when R.sup.6 is hydrogen, and R.sup.11 and R.sup.17a are hydroxy or when R.sup.6 is fluoro, R.sup.11 and R.sup.17a are hydroxyl and the dotted line in the 1,2-position together with the corresponding solid line denotes a single carbon-carbon bond, R.sup.9 is fluoro, chloro or bromo and processes for the preparation thereof are disclosed.
    Type: Grant
    Filed: December 26, 1978
    Date of Patent: May 13, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4197406
    Abstract: The present disclosure is concerned with 17a-(m-iodobenzoyloxy) substituted D-homosteroids and a process for their manufacture. The compounds are useful as intermediates and also as hormonal agents, particularly progestational agents.
    Type: Grant
    Filed: May 7, 1979
    Date of Patent: April 8, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4137269
    Abstract: The present disclosure relates to steroids. More particularly, the disclosure is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same. The subject D-homosteroids have high endocrinal activity and are particularly active as anti-inflammatory agents.
    Type: Grant
    Filed: October 12, 1976
    Date of Patent: January 30, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Klaus Kieslich, Rudolf Wiechert
  • Patent number: 4131655
    Abstract: D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.
    Type: Grant
    Filed: April 20, 1978
    Date of Patent: December 26, 1978
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4036874
    Abstract: D-homosteroids of the formula ##STR1## wherein R.sup.6 is hydrogen, fluorine, chlorine or methyl; R.sup.9 is hydrogen, fluorine, chlorine or bromine; R.sup.17 and R.sup.21 each independently are hydroxy or acyloxy, and U represents optional olefinic unsaturation are endocrine agents having anti-inflammatory properties.
    Type: Grant
    Filed: December 11, 1975
    Date of Patent: July 19, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller
  • Patent number: 4029692
    Abstract: The present disclosure relates to steroid carboxylic acids and derivatives thereof. More particularly, the disclosure is concerned with D-homosteroid carboxylic acids and their derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The instant compounds are active endocrinal agents, especially as antiinflammatory agents.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: June 14, 1977
    Inventors: Leo Alig, Robert Nickolson, Rudolf Wiechert, Andor Furst, Klaus Kieslich, Marcel Muller, Ulrich Kerb
  • Patent number: 4028400
    Abstract: The present invention relates to steroids. More particularly, the invention is concerned with D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same.
    Type: Grant
    Filed: September 20, 1974
    Date of Patent: June 7, 1977
    Inventors: Leo Alig, Andor Furst, Peter Keller, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4026923
    Abstract: A novel class of D-homosteroids is disclosed. These compounds have potent endocrinal activity, particularly as anti-inflammatory agents.
    Type: Grant
    Filed: November 6, 1975
    Date of Patent: May 31, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller
  • Patent number: 4026921
    Abstract: Novel D-homosteroids of the formula ##STR1## are disclosed. These compounds exhibit anti-inflammatory activity.
    Type: Grant
    Filed: September 20, 1974
    Date of Patent: May 31, 1977
    Inventors: Andor Furst, Marcel Muller, Leo Alig, Peter Keller, Ulrich Kerb, Rudolf Wiechert, Klaus Kieslich, Karl Petzoldt
  • Patent number: 4026918
    Abstract: Novel D-homosteroids of the formula ##STR1## are disclosed. The novel D-homosteroids exhibit anti-inflammatory activity and are useful intermediates for the synthesis of anti-inflammatory D-homosteroids.
    Type: Grant
    Filed: September 20, 1974
    Date of Patent: May 31, 1977
    Inventors: Andor Furst, Marcel Muller, Leo Alig, Peter Keller, Ulrich Kerb, Rudolf Wiechert, Klaus Kieslich, Karl Petzoldt
  • Patent number: 4026922
    Abstract: The present disclosure relates to novel D-homo-pregnene steroids useful as progestational agents.
    Type: Grant
    Filed: October 2, 1975
    Date of Patent: May 31, 1977
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 3965128
    Abstract: New 6.beta.,7.beta.-epoxy-17.alpha.-hydroxy or acyloxy-1.alpha.,2.alpha.-methylen-D-homo-4-pregnen-3,20-diones having surprising progestational activity are disclosed.
    Type: Grant
    Filed: September 23, 1974
    Date of Patent: June 22, 1976
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Marcel Muller, Leo Alig, Peter Keller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 3939193
    Abstract: A novel class of D-homosteroids is disclosed. These compounds have potent endocrinal activity, particularly as anti-inflammatory agents.
    Type: Grant
    Filed: August 29, 1974
    Date of Patent: February 17, 1976
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller